石胆酸腺苷的合成研究

Synthesis of Lithocholic Acid Adenosine

腺苷衍生物是由天然腺苷经过化学方法对糖基取代或修饰的一类化合物,具有抗癌、抗病毒、抗肿瘤,镇静、催眠等生理活性。甾体化合物石胆酸是一种次级胆汁酸,具有抑制肿瘤生长,杀死癌细胞等生理活性。本文以腺苷为起始原料,经氯硅烷保护羟基,选择性脱保护,酰基化,石胆酸酰胺化,脱硅基保护基五步合成石胆酸腺苷,总收率为9%。

Adenosine derivatives are natural adenosine chemically modified glycosyl group of compounds,with anti-cancer,anti-virus,anti-tumor,sedative,hypnotic and other physiological activities. Steroid Lithocholic acid is a secondary bile acid,with inhibition of tumor growth,killing cancer cells and other physiological activities. In this paper,Lithocholic acid adenosine was synthesized starting from adenosine via chlorosilane protection,selective deprotection,acylation,lithocholic acid amidation and deprotection with the total yield 9%.